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Jul 11,2023
Researchers developed a highly specific CDC7 inhibitor TAK-931 as a clinical cancer therapeutic agent. The antitumor efficacy studies were performed at Medicilon
Cell division cycle 7 (CDC7) plays important roles in DNA replication. Researchers developed a highly specific CDC7 inhibitor, TAK-931, as a clinical cancer therapeutic agent. The antitumor efficacy studies in PDX models were performed at Medicilon. Medicilon has established a complete evaluation system for preclinical anti-tumor efficacy, and has more than 200 different types of tumor efficacy models.
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Researchers developed a highly specific CDC7 inhibitor TAK-931 as a clinical cancer therapeutic agent. The antitumor efficacy studies were performed at Medicilon
Jul 11,2023
Pharmacological characterization of MT-1207, a novel multitarget antihypertensive agent. The binding inhibition activities of MT-1207 were evaluated by Medicilon
Hypertension is a serious public health problem worldwide. MT-1207 is a chemical entity that has entered into clinical trial as antihypertensive agent. MT-1207 potently inhibits adrenergic α1A, α1B, α1D, and 5-HT2A receptors with Ki < 1 nM in a panel of enzyme activity or radioligand binding assays. The binding inhibition activities of MT-1207 were evaluated by Medicilon.
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Pharmacological characterization of MT-1207, a novel multitarget antihypertensive agent. The binding inhibition activities of MT-1207 were evaluated by Medicilon
Jul 11,2023
Design, synthesis, and evaluation of potent RIPK1 inhibitors with in vivo anti-inflammatory activity. The PK parameters were determined at Medicilon
RIPK1 plays a key role in the necroptosis pathway that regulates inflammatory signaling and cell death in various diseases, including inflammatory and neurodegenerative diseases. Herein, researchers report a series of potent RIPK1 inhibitors, represented by compound 70. Compound 70 possesses favorable pharmacokinetic parameters with moderate clearance and good oral bioavailability in SD rat. The pharmacokinetic parameters were determined at Medicilon using male SD rats (3 rats per group, 4 groups).
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Design, synthesis, and evaluation of potent RIPK1 inhibitors with in vivo anti-inflammatory activity. The PK parameters were determined at Medicilon
Jul 11,2023
Discovery and synthesis of a new class of selective TNIK inhibitors and evaluation of their anti-colorectal cancer effects, the pharmacokinetic properties was carried out by Medicilon
The Traf2- and Nck-interacting protein kinase (TNIK) is a downstream signal protein of the Wnt/β-catenin pathway and has been thought of as a potential target for the treatment of colorectal cancer. SAR analysis leads to the identification of a number of potent TNIK inhibitors with Compound 21k being the most active one. Preliminary assessment for the pharmacokinetic properties of Compound 21k was carried out through services provided by Medicilon.
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Discovery and synthesis of a new class of selective TNIK inhibitors and evaluation of their anti-colorectal cancer effects, the pharmacokinetic properties was carried out by Medicilon
Jul 11,2023
Design, synthesis, and biological evaluation of potent PPARα/δ dual agonists for the treatment of nonalcoholic steatohepatitis. The PK studies, hERG studies, and Ames tests were conducted by Medicilon
Nonalcoholic steatohepatitis (NASH) is the advanced subtype of nonalcoholic fatty liver disease (NAFLD) and is becoming a severe global public health problem. PPARα/δ are regarded as potential therapeutic targets for NASH. Herein, researchers report a series of novel triazolone derivatives as PPARα/δ dual agonists. The pharmacokinetic studies were conducted by Medicilon. The hERG channel inhibition studies were conducted by Medicilon. The Ames tests were conducted by Medicilon.
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Design, synthesis, and biological evaluation of potent PPARα/δ dual agonists for the treatment of nonalcoholic steatohepatitis. The PK studies, hERG studies, and Ames tests were conducted by Medicilon
Jul 11,2023
ARD-2585 is an orally active PROTAC degrader of androgen receptor for the treatment of advanced prostate cancer
A PROTAC-based androgen receptor (AR) degrader is a bifunctional small molecule, consisting of an AR ligand that binds to AR protein, and a ligand that binds to and recruits an E3 ligase complex, tethered together through a linker. Researchers report the discovery of exceptionally potent and orally bioavailable PROTAC AR degrader ARD-2585 (Compound 43). ARD-2585 is a promising AR degrader for extensive investigations for the treatment of advanced prostate cancer. The liver microsomal stability assay was performed by Medicilon. The plasma stability assay was performed by Medicilon. The hERG assay was performed by Medicilon.
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ARD-2585 is an orally active PROTAC degrader of androgen receptor for the treatment of advanced prostate cancer
Jul 11,2023
A selective c-Myc degrader potently regresses lethal c-Myc overexpressing tumors. SPR experiments were performed by Medicilon
Cancer is one of the leading causes of death worldwide. MYC oncogene is involved in the majority of human cancers and is often associated with poor outcomes. WBC100, a novel oral active molecule glue that selectively degrades c‐Myc protein over other proteins and potently kills c‐Myc overexpressing cancer cells is reported. Researchers performed direct binding assay of WBC100 with c-Myc on biosensor chip by surface plasmon resonance (SPR). SPR experiments were performed using a Biacore T200 instrument by Medicilon.
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A selective c-Myc degrader potently regresses lethal c-Myc overexpressing tumors. SPR experiments were performed by Medicilon
Jun 26,2023
Medicilon congratulates MindRank's GLP-1RA small molecule oral drug for successfully administering the first subject in clinical phase I
MindRank's GLP-1RA small molecule oral drug has been successfully administered to the first subject in clinical phase I. Medicilon as a strategic partner of MindRank, provided MDR-001 with API process development and preparation R&D services to help speed up its research and development.
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Medicilon congratulates MindRank's GLP-1RA small molecule oral drug for successfully administering the first subject in clinical phase I
Jun 21,2023
Medicilon Assists Toll Biotech's TollB-001 tablets, a new class 1.1 drug, to officially approve for clinical trials by the FDA
Recently, the IND application of TollB-001 Tablets, a class 1.1 new drug for rheumatoid arthritis by Toll Biotech, has been officially approved by the FDA. Medicilon provided pharmaceutical research services, including raw materials and preparation, for TollB-001 tablets, which accelerated the research process.
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Medicilon Assists Toll Biotech's TollB-001 tablets, a new class 1.1 drug, to officially approve for clinical trials by the FDA
Jun 14,2023
Congratulations on the positive phase I clinical results of Raymon Pharma's first Chinese eye drops for the treatment of wAMD
Recently, Raymon Pharma announced that the clinical trial of self-developed RA1115-B1 eye drops for the treatment of neovascular (wet) age-related macular degeneration (wAMD) was launched in China. Medicilon provided pharmaceutical research services such as raw material drug production, raw material drug process development, and preparation prescription process development to accelerate the R&D process.
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Congratulations on the positive phase I clinical results of Raymon Pharma's first Chinese eye drops for the treatment of wAMD